Bacterial resistance to currently available antibiotics is becoming increasingly frequent in both the hospital setting and the community. Multi-drug or even pan-drug resistance, i.e. resistance to nearly all available antibiotic classes (e.g. beta-lactams, quinolones, tetracyclines, glycopeptides and macrolides), is rapidly emerging in clinically relevant pathogens. This important clinical problem, together with the lack of investment in the discovery and development of new antibiotic treatments active on multi-drug resistant pathogens, especially Gram-negative bacteria, thus represents a relevant Public Health issue and medical need [1].
The prevalence and severity of antibiotic resistance (AR) is becoming evident worldwide and is associated with increased morbidity and mortality of infectious diseases, thus creating a huge socio-economic burden on Public Healthcare systems [1], [2].
Then, there is the need for compounds endowed with activity against both Gram-negative and Gram-positive bacteria.
Documents U.S. Pat. No. 3,499,927, WO2008/029810 and WO2006/118283 relates to guanidine derivatives of polyalkylene polyamines useful against bacteria infecting humans or against plant pathogenic fungi.
Manetti et al.[3] disclose guanidine compounds having affinity as competitive inhibitors of maize polyamine oxidase. Such compounds are interesting to inhibit cell proliferation, in particular in tumor cell lines.
The document WO2009/113033 discloses linear and cyclic guanidine derivatives for use as anti-infectious agents.